R. Fuller
Oct 1, 1968
Citations
0
Influential Citations
57
Citations
Quality indicators
Journal
Biochemical pharmacology
Abstract
Abstract N -[2-( o -chlorophenoxy)-ethyl]-cyclopropylamine (51641) and related compounds inhibited the oxidation by monoamine oxidase (MAO) of serotonin, tyramine, phenethylamine and tryptamine in vitro . The inhibition by 51641 was noncompetitive. By using kynuramine as substrate to study reaction rates, it was found that inhibition by 51641 was maximum at pH 7.5, increased with time of incubation of enzyme and inhibitor, was not reversible by dialysis and was independent of enzyme concentration. In vivo , 51641 increased the amount of serotonin in the whole brain of the rat. Urinary excretion of tryptamine by rats, dogs and human subjects was increased after administration of 51641. Compound 51641 thus is a potent inhibitor of MAO in vitro and in vivo .